A phase II prospective open-label escalating dose trial of recombinant interleukin-11 in mild von Willebrand disease

Haemophilia. 2008 Sep;14(5):968-77. doi: 10.1111/j.1365-2516.2008.01827.x. Epub 2008 Aug 1.

Abstract

von Willebrand factor (VWF) is a multimeric glycoprotein that mediates platelet adhesion and is decreased in von Willebrand disease (VWD). 1-8 deamino-d-arginine vasopressin (DDAVP), the most common treatment for VWD, is limited by tachyphylaxis and inconvenience, and in 20% of the patients, unresponsiveness. Recombinant human interleukin-11 (rhIL-11), a gp-130 signalling cytokine with haematopoietic and anti-inflammatory activity, increases VWF antigen and its activity in heterozygous VWF(+/-) mice and dogs. To determine the biological efficacy and safety of rhIL-11 in non-bleeding human subjects with mild VWD, we conducted a phase II prospective open-label trial of rhIL-11 at 10, 25 and 50 mug kg(-1) subcutaneously (s.c.), given daily for 7 days in nine subjects with mild VWD. VWF and factor VIII (FVIII) levels increased gradually and progressively after s.c. rhIL-11, which was sustained through 7 days of dosing to 1.5- to 3-fold over baseline. Following intravenous DDAVP, 0.3 mug kg(-1), on day 7 there was a further boost in VWF and FVIII levels, suggesting that the mechanism of rhIL-11 differs from that of DDAVP. Platelet VWF mRNA expression measured by quantitative PCR increased from two- to eightfold over baseline, suggesting that the mechanism of rhIL-11 effect may be upregulation of VWF mRNA. VWF and FVIII levels returned to baseline by day 14. rhIL-11 was well tolerated with less than grade-1 hypertension, hypokalaemia and fluid retention. Recombinant IL-11 increases VWF levels in humans with mild VWD, justifying future clinical trials to determine its potential in preventing or reducing bleeding in this patient population.

Publication types

  • Clinical Trial, Phase II

MeSH terms

  • Adult
  • Deamino Arginine Vasopressin / adverse effects
  • Deamino Arginine Vasopressin / therapeutic use
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Factor VIII / metabolism
  • Female
  • Hemostatics / adverse effects
  • Hemostatics / therapeutic use
  • Humans
  • Injections, Subcutaneous
  • Interleukin-11 / administration & dosage*
  • Interleukin-11 / adverse effects
  • Interleukin-11 / therapeutic use
  • Male
  • Platelet Count
  • Polymerase Chain Reaction / methods
  • Prospective Studies
  • RNA, Messenger / genetics
  • Recombinant Proteins / therapeutic use
  • Young Adult
  • von Willebrand Diseases / blood
  • von Willebrand Diseases / drug therapy*
  • von Willebrand Factor / biosynthesis
  • von Willebrand Factor / genetics
  • von Willebrand Factor / metabolism

Substances

  • Hemostatics
  • Interleukin-11
  • RNA, Messenger
  • Recombinant Proteins
  • von Willebrand Factor
  • Factor VIII
  • Deamino Arginine Vasopressin